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Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase.

ABSTRACT: We report herein the discovery of a fatty acid amide hydrolase (FAAH) positron emission tomography (PET) tracer. Starting from a pyrazole lead, medicinal chemistry efforts directed toward reducing lipophilicity led to the synthesis of a series of imidazole analogues. Compound 6 was chosen for further profiling due to its appropriate physical chemical properties and excellent FAAH inhibition potency across species. [(11)C]-6 (MK-3168) exhibited good brain uptake and FAAH-specific signal in rhesus monkeys and is a suitable PET tracer for imaging FAAH in the brain.

SUBMITTER: Liu P 

PROVIDER: S-EPMC4027136 | biostudies-literature | 2013 Jun

REPOSITORIES: biostudies-literature

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Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase.

Liu Ping P   Hamill Terence G TG   Chioda Marc M   Chobanian Harry H   Fung Selena S   Guo Yan Y   Chang Linda L   Bakshi Raman R   Hong Qingmei Q   Dellureficio James J   Lin Linus S LS   Abbadie Catherine C   Alexander Jessica J   Jin Hong H   Mandala Suzanne S   Shiao Lin-Lin LL   Li Wenping W   Sanabria Sandra S   Williams David D   Zeng Zhizhen Z   Hajdu Richard R   Jochnowitz Nina N   Rosenbach Mark M   Karanam Bindhu B   Madeira Maria M   Salituro Gino G   Powell Joyce J   Xu Ling L   Terebetski Jenna L JL   Leone Joseph F JF   Miller Patricia P   Cook Jacquelynn J   Holahan Marie M   Joshi Aniket A   O'Malley Stacey S   Purcell Mona M   Posavec Diane D   Chen Tsing-Bau TB   Riffel Kerry K   Williams Mangay M   Hargreaves Richard R   Sullivan Kathleen A KA   Nargund Ravi P RP   DeVita Robert J RJ  

ACS medicinal chemistry letters 20130420 6

We report herein the discovery of a fatty acid amide hydrolase (FAAH) positron emission tomography (PET) tracer. Starting from a pyrazole lead, medicinal chemistry efforts directed toward reducing lipophilicity led to the synthesis of a series of imidazole analogues. Compound 6 was chosen for further profiling due to its appropriate physical chemical properties and excellent FAAH inhibition potency across species. [(11)C]-6 (MK-3168) exhibited good brain uptake and FAAH-specific signal in rhesus  ...[more]

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